Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
Kung, P.P., Bingham, P., Brooun, A., Collins, M., Deng, Y.L., Dinh, D., Fan, C., Gajiwala, K.S., Grantner, R., Gukasyan, H.J., Hu, W., Huang, B., Kania, R., Kephart, S.E., Krivacic, C., Kumpf, R.A., Khamphavong, P., Kraus, M., Liu, W., Maegley, K.A., Nguyen, L., Ren, S., Richter, D., Rollins, R.A., Sach, N., Sharma, S., Sherrill, J., Spangler, J., Stewart, A.E., Sutton, S., Uryu, S., Verhelle, D., Wang, H., Wang, S., Wythes, M., Xin, S., Yamazaki, S., Zhu, H., Zhu, J., Zehnder, L., Edwards, M.
J. Med. Chem.